Rociletinib (Synonyms: CO-1686; AVL-301; CNX-419)

Name: Rociletinib
Brand: MedChemExpress
SKU: HY-15729
Rating: 5.0 (15 reviews)

Cat. No.: HY-15729 Purity: 99.79%: FAQs
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Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the K_i values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.

For research use only. We do not sell to patients.

Rociletinib Chemical Structure

CAS No. : 1374640-70-6

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 15 publication(s) in Google Scholar

Other Forms of Rociletinib:

Rociletinib hydrobromide In-stock

13 Publications Citing Use of MCE Rociletinib

RT-PCR

: Rociletinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 May;10(5):799-811. [Abstract]; The protein level of ABCG2 on MDR cells after 0, 0.25, 0.5 and 1 µmol/L rociletinib stimulation for 48 h are measured by Western blot analysis.

: Rociletinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 May;10(5):799-811. [Abstract]; Rociletinib enhances the anticancer effect of topotecan in the S1-MI-80 tumor xenograft model in nude mice. (A)The changes in tumor volume over time after the S1-MI-80 cell implantation (n=6). Data shown are mean±SD of tumor volumes for each group. (B) The image of tumors size in four groups excised from the mice on the 75th day after implantation.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

EGFR^L858R/T790M

21.5 nM (Ki)

EGFR^T790M

303.3 nM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	> 4331 nM Compound: CO-1686	Inhibition of wild type EGFR phosphorylation in human A431 cells after 1 hr by Western blot analysis Inhibition of wild type EGFR phosphorylation in human A431 cells after 1 hr by Western blot analysis	[PMID: 26968253]
A-431	IC₅₀	1.29 μM Compound: 4	Antiproliferative activity against wild type human A431 cells after 48 hrs by MTT assay Antiproliferative activity against wild type human A431 cells after 48 hrs by MTT assay	[PMID: 27634676]
A-431	IC₅₀	1.29 μM Compound: Rociletinib	Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
A-431	IC₅₀	1.545 μM Compound: 2	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay	[PMID: 28033579]
A-431	EC₅₀	1.66 μM Compound: Rociletinib	Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
A-431	IC₅₀	1.79 μM Compound: Rociletinib	Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as decrease in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28385595]
A-431	IC₅₀	1.794 μM Compound: 5	Antiproliferative activity against human A431 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A431 cells incubated for 72 hrs by MTT assay	[PMID: 28395219]
A-431	GI₅₀	547 nM Compound: CO-1686	Antiproliferative activity against wild type EGFR expressing human A431 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis Antiproliferative activity against wild type EGFR expressing human A431 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis	[PMID: 26968253]
A-431	IC₅₀	6.01 μM Compound: Rociletinib	Antiproliferation activity against human A431 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay Antiproliferation activity against human A431 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay	[PMID: 32912431]
A-431	IC₅₀	641 nM Compound: 5; CO-1686	Cytotoxicity against human A431 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by SRB assay Cytotoxicity against human A431 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 29906114]
A549	IC₅₀	1600 nM Compound: 8; CO-1686	Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA	[PMID: 26756222]
A549	IC₅₀	3.24 μM Compound: Rociletinib	Antiproliferative activity against human A549 cells harboring EGFR K-ras mutant assessed as decrease in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring EGFR K-ras mutant assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28385595]
A549	IC₅₀	3.242 μM Compound: 5	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 28395219]
A549	IC₅₀	6.5 μM Compound: Rociletinib	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
A549	IC₅₀	6.502 μM Compound: 4	Antiproliferative activity against human A549 cells harboring K-ras mutation after 48 hrs by MTT assay Antiproliferative activity against human A549 cells harboring K-ras mutation after 48 hrs by MTT assay	[PMID: 27634676]
A549	IC₅₀	7.57 μM Compound: CO-1686	Anti-proliferative activity against human A549 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay Anti-proliferative activity against human A549 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35594654]
BaF3	GI₅₀	0.94 μM Compound: 4; C01686	Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28282122]
COS-7	IC₅₀	7.39 μM Compound: Rociletinib	Cytotoxicity against African green monkey COS7 cells assessed as decrease in cell viability incubated incubated for 48 hrs by MTT assay Cytotoxicity against African green monkey COS7 cells assessed as decrease in cell viability incubated incubated for 48 hrs by MTT assay	[PMID: 32912431]
HaCaT	IC₅₀	262.3 nM Compound: 6; CO-1686	Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method	[PMID: 27433829]
HCC827	GI₅₀	0.03 μM Compound: CO-1686	Growth inhibition of human HCC827 cells with exon 19 deletion and delE746-A750 incubated for 96 hrs by cell-titer Glo reagent based assay Growth inhibition of human HCC827 cells with exon 19 deletion and delE746-A750 incubated for 96 hrs by cell-titer Glo reagent based assay	[PMID: 26275028]
HCC827	IC₅₀	0.031 μM Compound: Rociletinib	Antiproliferative activity against human HCC827 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
HCC827	IC₅₀	0.031 μM Compound: 5	Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay	[PMID: 28395219]
HCC827	IC₅₀	0.031 μM Compound: Rociletinib	Antiproliferative activity against human HCC827 cells harboring EGFR del E746 to A750 mutant assessed as decrease in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells harboring EGFR del E746 to A750 mutant assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28385595]
HCC827	EC₅₀	0.045 μM Compound: Rociletinib	Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
HCC827	GI₅₀	7 nM Compound: CO-1686	Antiproliferative activity against EGFR Del 19 mutant expressing human HCC827 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis Antiproliferative activity against EGFR Del 19 mutant expressing human HCC827 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis	[PMID: 26968253]
NCI-H1975	GI₅₀	0.03 μM Compound: CO-1686	Growth inhibition of human NCI-H1975 cells expressing EGFR L858R/T790M mutant incubated for 96 hrs by cell-titer Glo reagent based assay Growth inhibition of human NCI-H1975 cells expressing EGFR L858R/T790M mutant incubated for 96 hrs by cell-titer Glo reagent based assay	[PMID: 26275028]
NCI-H1975	IC₅₀	0.042 μM Compound: 2	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay	[PMID: 28033579]
NCI-H1975	EC₅₀	0.1 μM Compound: Rociletinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
NCI-H1975	IC₅₀	0.13 μM Compound: CO-1686	Anti-proliferative activity against human NCI-H1975 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay Anti-proliferative activity against human NCI-H1975 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35594654]
NCI-H1975	IC₅₀	0.137 μM Compound: 4	Antiproliferative activity against human NCI-H1975 cells harboring L858R/T790M double mutant after 48 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring L858R/T790M double mutant after 48 hrs by MTT assay	[PMID: 27634676]
NCI-H1975	IC₅₀	0.137 μM Compound: Rociletinib	Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
NCI-H1975	IC₅₀	0.137 μM Compound: Rociletinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as decrease in cell viability after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28385595]
NCI-H1975	IC₅₀	0.299 μM Compound: 5	Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay	[PMID: 28395219]
NCI-H1975	IC₅₀	0.51 μM Compound: Rociletinib	Antiproliferation activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay Antiproliferation activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay	[PMID: 32912431]
NCI-H1975	IC₅₀	16 nM Compound: 8; CO-1686	Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA	[PMID: 26756222]
NCI-H1975	IC₅₀	31 nM Compound: 5; CO-1686	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay	[PMID: 29906114]
NCI-H1975	IC₅₀	62 nM Compound: CO-1686	Inhibition of EGFR L858R / T790M double mutant phosphorylation in human NCI-H1975 cells after 1 hr by Western blot analysis Inhibition of EGFR L858R / T790M double mutant phosphorylation in human NCI-H1975 cells after 1 hr by Western blot analysis	[PMID: 26968253]
NCI-H1975	GI₅₀	7 nM Compound: CO-1686	Antiproliferative activity against EGFR L858R / T790M double mutant expressing human NCI-H1975 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis Antiproliferative activity against EGFR L858R / T790M double mutant expressing human NCI-H1975 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis	[PMID: 26968253]
NCI-H358	IC₅₀	> 2000 nM Compound: CO-1686	Inhibition of wild type EGFR phosphorylation in human NCI-H358 cells after 1 hr by Western blot analysis Inhibition of wild type EGFR phosphorylation in human NCI-H358 cells after 1 hr by Western blot analysis	[PMID: 26968253]
NCI-H661	GI₅₀	1.7 μM Compound: CO-1686	Growth inhibition of human NCI-H661 cells incubated for 96 hrs by cell-titer Glo reagent based assay Growth inhibition of human NCI-H661 cells incubated for 96 hrs by cell-titer Glo reagent based assay	[PMID: 26275028]
PC-9	IC₅₀	0.27 μM Compound: CO-1686	Anti-proliferative activity against human PC-9 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay Anti-proliferative activity against human PC-9 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35594654]
PC-9	IC₅₀	211 nM Compound: CO-1686	Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells after 1 hr by Western blot analysis Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells after 1 hr by Western blot analysis	[PMID: 26968253]
PC-9	GI₅₀	7 nM Compound: CO-1686	Antiproliferative activity against EGFR Del ex19 mutant expressing human PC9 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis Antiproliferative activity against EGFR Del ex19 mutant expressing human PC9 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis	[PMID: 26968253]
PC-9	IC₅₀	79 nM Compound: 8; CO-1686	Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA	[PMID: 26756222]
Sf9	IC₅₀	0.002 μM Compound: CO-1686	Inhibition of wild type EGFR (unknown origin) expressed in Sf9 cells pre-incubated for 30 mins before substrate and ATP addition by homogeneous time-resolved FRET assay Inhibition of wild type EGFR (unknown origin) expressed in Sf9 cells pre-incubated for 30 mins before substrate and ATP addition by homogeneous time-resolved FRET assay	[PMID: 26275028]
Sf9	IC₅₀	0.002 μM Compound: CO-1686	Inhibition of EGFR L858R mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay Inhibition of EGFR L858R mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay	[PMID: 26275028]
Sf9	IC₅₀	0.003 μM Compound: CO-1686	Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay	[PMID: 26275028]
Sf9	IC₅₀	21.5 nM Compound: 4	Inhibition of human recombinant N-terminal GST-tagged EGFR T790M/L858R double mutant cytoplasmic domain (695 end residues) autophosphorylation expressed in baculovirus infected Sf9 insect cells by ADP-Glo luminescence assay Inhibition of human recombinant N-terminal GST-tagged EGFR T790M/L858R double mutant cytoplasmic domain (695 end residues) autophosphorylation expressed in baculovirus infected Sf9 insect cells by ADP-Glo luminescence assay	[PMID: 27634676]
Sf9	IC₅₀	460 nM Compound: 4	Inhibition of human recombinant N-terminal GST-tagged wild type EGFR cytoplasmic domain (695 end residues) autophosphorylation expressed in baculovirus infected Sf9 insect cells by ADP-Glo luminescence assay Inhibition of human recombinant N-terminal GST-tagged wild type EGFR cytoplasmic domain (695 end residues) autophosphorylation expressed in baculovirus infected Sf9 insect cells by ADP-Glo luminescence assay	[PMID: 27634676]
SW-620	IC₅₀	10.5 μM Compound: Rociletinib	Antiproliferation activity against EGFR-negative human SW620 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay Antiproliferation activity against EGFR-negative human SW620 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay	[PMID: 32912431]

In Vitro

Rociletinib (CO-1686) (0.1 μM) inhibits EGFR potently and irreversibly, and inhibits more than 50% of 23 targets. Rociletinib potently and selectively inhibits growth of NSCLC cells expressing mutant EGFR and induces apoptosis. Rociletinib resistant NSCLC cell lines are sensitive to AKT inhibition^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Rociletinib (CO-1686) (100 mg/kg/day, p.o.) demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft models. Rociletinib (CO-1686) (50 mg/kg bid, p.o.) demonstrates anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

555.55

Formula

C₂₇H₂₈F₃N₇O₃

CAS No.

1374640-70-6

Appearance

Solid

Color

White to off-white

SMILES

C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(N4CCN(C(C)=O)CC4)C=C3OC)=NC=C2C(F)(F)F)=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (225.00 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8000 mL	9.0001 mL	18.0002 mL
5 mM	0.3600 mL	1.8000 mL	3.6000 mL
10 mM	0.1800 mL	0.9000 mL	1.8000 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.79%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (248 KB) LCMS (266 KB)

Handling Instructions (2659 KB)

References

[1]. Walter AO, et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013 Sep 25. [Content Brief]

Cell Assay ^[1]	Cells are seeded at 3,000 cells/well in growth media supplemented with 5% FBS, 2 mM L-glutamine, and 1 % P/S, allowed to adhere overnight, and treated with a dilution series of test compound (Rociletinib) for 72 hr. Cell viability is determined by CellTiter Glo and results are represented as background-subtracted relative light units normalized to a DMSO-treated control. Growth inhibition (GI₅₀) values are determined by GraphPad Prism 5.04. Combination index (CI) data is generated using CalcuSyn. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Briefly, NCr nu/nu mice are sub-cutaneously implanted with 1×10⁷ tumor cells in 50% Matrigel (injection volume of 0.2 mL/mouse). Once tumors reached 100-200 mm³, Animals are dosed with compounds (Rociletinib) as outlined (N=10 animals/gp). Briefly, LUM1686 PDX tumor fragments, harvested from donor mice, are inoculated into BALB/c nude mice. Administration of test compounds (Rociletinib (CO-1686)) is initiated at a mean tumor size of approximately 160 mm³. Tumor growth is monitored over time to determine tumor growth inhibition of the experimental agent vs. vehicle. The endpoint of the experiment is a mean tumor volume (MTV) in control group of 2000 mm³. Percent TGI is defined as the difference between the MTV of the designated control group and the MTV of the drug-treated group, expressed as a percentage of the MTV of the designated control group. Data is presented as mean±standard error of the mean (SEM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Walter AO, et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013 Sep 25. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.8000 mL	9.0001 mL	18.0002 mL	45.0005 mL
	5 mM	0.3600 mL	1.8000 mL	3.6000 mL	9.0001 mL
	10 mM	0.1800 mL	0.9000 mL	1.8000 mL	4.5000 mL
	15 mM	0.1200 mL	0.6000 mL	1.2000 mL	3.0000 mL
	20 mM	0.0900 mL	0.4500 mL	0.9000 mL	2.2500 mL
	25 mM	0.0720 mL	0.3600 mL	0.7200 mL	1.8000 mL
	30 mM	0.0600 mL	0.3000 mL	0.6000 mL	1.5000 mL
	40 mM	0.0450 mL	0.2250 mL	0.4500 mL	1.1250 mL
	50 mM	0.0360 mL	0.1800 mL	0.3600 mL	0.9000 mL
	60 mM	0.0300 mL	0.1500 mL	0.3000 mL	0.7500 mL
	80 mM	0.0225 mL	0.1125 mL	0.2250 mL	0.5625 mL
	100 mM	0.0180 mL	0.0900 mL	0.1800 mL	0.4500 mL

Rociletinib Related Classifications

Help & FAQs

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Rociletinib (Synonyms: CO-1686; AVL-301; CNX-419)

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Other Forms of Rociletinib:

13 Publications Citing Use of MCE Rociletinib

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Purity & Documentation

References

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Complete Stock Solution Preparation Table

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Rociletinib (Synonyms: CO-1686; AVL-301; CNX-419)

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